4″′-N-Demethylspiramycin Derivatives: Synthesis and Evaluation of Effectiveness against Drug-resistant Bacteria

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Abstract

18-Amino-4″-O-benzoyl-4″′-N-demethyl-18-deoxospiramycins were designed and synthesized. Synthetic strategy involved selective demethylation of the dimethylamino group in forosamine, benzoylation of the hydroxyl group at the C4″ position and reductive N-amination of the formyl group. Antibacterial characteristics of spiramycin derivatives were tested. The derivatives exhibited promising activity against drug-resistant bacterial strains.

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Correspondence to Satoshi Ōmura.

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Keywords

  • spiramycin
  • MRSA
  • demethylation
  • reductive N-amination

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